Target intelligence / Profile preview

Vascular endothelial growth factor receptor 1, Vascular endothelial growth factor receptor 2, Platelet-derived growth factor receptor alpha, Platelet-derived growth factor receptor beta (VEGFR1, VEGFR2, PDGFRα, PDGFRβ)

Target
VEGFR1, VEGFR2, PDGFRα, PDGFRβ
Molecular classification
Receptor tyrosine kinase, Receptor, Enzyme (specifically, kinase superfamily)
01

Overview

Vascular endothelial growth factor receptors 1 and 2 (VEGFR1, VEGFR2) and platelet-derived growth factor receptors alpha and beta (PDGFRα, PDGFRβ) are receptor tyrosine kinases that function as key regulators of vascular development, angiogenesis, and cell proliferation. VEGFR1 and VEGFR2 bind vascular endothelial growth factors, activating intracellular signaling cascades mediating endothelial cell proliferation, survival, and migration. PDGFRα and PDGFRβ bind platelet-derived growth factors, promoting mesenchymal cell proliferation, migration, and survival. These receptors are highly relevant in tumor angiogenesis and are frequent therapeutic targets in cancer, ophthalmology, and other proliferative diseases. Their dysregulation contributes to oncogenesis, inflammation, fibrosis, and angiogenic eye diseases[1][2][3]. If you require structured information on only one of these targets, separate entries should be used for each molecule.

Other names
Flt-1KDR (human)Flk-1 (mouse)CD140aCD140b
02

Mechanism of action

Inhibition of receptor tyrosine kinase activity, preventing downstream signaling in angiogenesis, cell proliferation, and survival. Ligand (VEGF/PDGF) binding blockade (for antibody drugs). Multi-kinase inhibition (most small molecules).

03

Biological functions

Signal transductionRegulation of angiogenesis and vascular permeabilityCell proliferation and survivalCell migration/differentiation
04

Disease associations

Cancer (e.g., solid tumors, leukemia)Cardiovascular diseaseInflammationFibrotic diseaseOcular diseases (e.g., macular degeneration)
05

Safety considerations

HypertensionProteinuriaHemorrhage/bleeding riskImpaired wound healingCardiovascular adverse events (e.g., heart failure, thromboembolism)Myelosuppression (for some multi-targeted inhibitors)
06

Interacting drugs

Sorafenib

6 more in the full profile.

07

Biomarkers

Receptor expression (IHC, mRNA for VEGFR1, VEGFR2, PDGFRα/β)Phosphorylation/activation status of the receptorsCirculating VEGF/PDGF ligand levels

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